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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2020-03-18
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Clobetasol propionate residues as well as
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Taken together our results demonstrate that the
2020-03-18
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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br Results and discussion br Conclusion In
2020-03-18
Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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It is not precisely known which of the
2020-03-18
It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH3
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Diagnosis of NCC can be accomplished via imaging techniques
2020-03-18
Diagnosis of NCC can be accomplished via imaging techniques and serological confirmatory testing. The best immunodiagnostic test for NCC, the enzyme-linked immunotransfer blot EITB (Tsang et al., 1989), is based on the detection of gsk-3 to one or more of the 7 lentil-lectin glycoproteins (LLGP) of
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Contrary to the profuse dopaminergic innervation of the thal
2020-03-18
Contrary to the profuse dopaminergic innervation of the thalamus found in human and non-human primates (Brown et al., 1979, Sanchez-Gonzalez et al., 2005), in rodents, the RTn is one the few thalamic nuclei that receives dopaminergic input (Anaya-Martinez et al., 2006, Garcia-Cabezas et al., 2007, G
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We have previously reported DAPK inhibitors
2020-03-18
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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As compared with the broad
2020-03-17
As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile hmg-coa reductase inhibitors LCA. Recently, the VDR-binding capacities of more compounds
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Regarding the mechanism of action
2020-03-17
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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Located on the fore tarsals of the front pair
2020-03-17
Located on the fore-tarsals of the front pair of legs, the Haller’s organ is presumed central to tick chemosensation. Recent genomic, transcriptomic and proteomic investigations have identified several families of transmembrane proteins in the forelegs of ticks that are likely involved in olfactory
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Paroxetine HCl Significantly elevated levels of DNA damage o
2020-03-17
Significantly elevated levels of DNA damage observed in peripheral blood of tea garden women workers indicate the occupational exposure. The same was observed in cholinesterase activities, which detected lower activity in the exposed group compared to non-exposed. Large volumes of pesticides are use
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Converging evidence suggests that reduced glutamate transmis
2020-03-17
Converging evidence suggests that reduced glutamate transmission in the LS is linked to increased anxiety-like behaviors (Radulovic et al., 1999, Henry et al., 2006, Bakshi et al., 2002, Liu et al., 2004). Therefore, attenuated CRF1 receptor-mediated excitatory transmission in the LS following ASV-t
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br Materials and methods br Results br Discussion Adiponecti
2020-03-17
Materials and methods Results Discussion Adiponectin is one of the most studied adipocytokines. Its release from adipocytes is down-regulated in obesity and other adverse metabolic conditions leading to decreased serum concentrations (Turer and Scherer, 2012). Several factors and conditions
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More recently it was discovered that BChE
2020-03-17
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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It has been reported that Eph Ephrin are involved in
2020-03-17
It has been reported that Eph/Ephrin are involved in the regulation of the tumor angiogenesis [10], [11], [12]. The distinct and specific involvement of Orlistat mg and veins in tumor angiogenesis is unclear. EphrinB2 is expressed in arteries and its receptor EphB4 is expressed in veins; these molec
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